Kissei Pharmaceutical Co., Ltd.

Yasunori Ueno

Masako Yoshida

Takashi Miyagi

Kazuo Shimizu

Kohsuke Ohno

Hikaru Suzuki

Toshihiro Nishimura

Nobuyuki Tanaka

Takehiro Ishikawa

Kiyoshi Kasai

Hitoshi Inoue

Satoko Kobayashi

Hirotaka Teranishi

Hiroaki Shiohara

Yusuke Onda

The present invention provides a new compound which has NKreceptor antagonist activity, whose CYP3A4 inhibitory activity is reduced compared to aprepitant, and which are useful for the prevention or treatment of cancer-chemotherapy-induced nausea and vomiting. That is, the present invention relates to carboxymethyl piperidine derivatives represented by the following formula (I) or a pharmaceutically acceptable salt thereof. Wherein, ring A is a benzene ring or the like; ring B is a pyridine ring or the like; Ris Calkyl or Calkoxy; Rand Rare a hydrogen atom or methyl; and n is an integral number from 0 to 5. 

Carboxymethyl piperidine derivative

A problem of the present invention is to provide a new compound which has NKreceptor antagonist activity, whose CYP3A4 inhibitory activity is reduced compared to aprepitant, and which are useful for the prevention or treatment of cancer-chemotherapy-induced nausea and vomiting. That is, the present invention relates to cyclohexyl pyridine derivatives represented by the following formula (I) or a pharmaceutically acceptable salt thereof, wherein, ring A is 4-fluoro-2-methylphenyl or the like; X is a hydrogen atom or the like; Ris carboxymethyl or the like; Ris alkyl or the like; Y is 0-2 or the like; U is &#x2014;N(CH)COC(CH)-3,5-bistrifluoromethylphenyl or the like. 

Cyclohexyl pyridine derivative

A problem of the present invention is to provide a new compound which has NKreceptor antagonist activity, whose CYP3A4 inhibitory activity is reduced compared to aprepitant, and which are useful for the prevention or treatment of cancer-chemotherapy-induced nausea and vomiting. That is, the present invention relates to cyclohexyl pyridine derivatives represented by the following formula (I) or a pharmaceutically acceptable salt thereof. wherein, ring A is 4-fluoro-2-methylphenyl or the like; X is a hydrogen atom or the like; Ris carboxymethyl or the like; Ris alkyl or the like; Y is 0-2 or the like; U is &#x2014;N(CH)COC(CH)-3,5-bistrifluoromethylphenyl or the like. 

[Problem] To provide a novel compound that exhibits an agonistic effect on dopamine Dreceptors. [Solution] The present invention provides a compound represented by the general formula (I): in which Ris Calkyl or the like; Ris hydrogen or the like; Rand Rare each hydrogen, Calkyl, RRN&#x2014;Calkyl, aralkyl, or the like; Rand Rare hydrogen or the like; and Ris hydrogen or the like, or a pharmaceutically acceptable salt thereof, a pharmaceutical compositions containing same and uses for said compound/salt and composition. The compounds of the present invention exhibit potent dopamine Dreceptor simulating activities and thus are useful as a treating or preventing agent for Parkinson's disease and the like.

[object Object]

The present invention provides compounds represented by the general formula (I): or pharmaceutical acceptable salts thereof, wherein Ris cyano or the like; Rand Rare hydrogen or the like; Ris Calkyl or the like; Ris Calkyl, halo-Calkyl, cycloalkyl, cycloalkyl-Calkyl, aralkyl or the like; Rand Rare each hydrogen, Calkyl, halo-Calkyl, cycloalkyl, Calkoxy-Calkyl, RRN&#x2014;Calkyl or the like, which exhibit potent dopamine Dreceptor stimulating activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof. 

Octahydrothienoquinoline derivative, pharmaceutical composition comprising derivative, and use of these

The present invention provides compounds represented by general formula (I): or pharmaceutical acceptable salts thereof, wherein Rand Rare each hydrogen, lower acyl, lower alkoxycarbonyl or the like; Ris lower alkyl, halo-lower alkyl, cycloalkyl, heterocycloalkyl, optionally substituted aryl, optionally substituted heteroaryl or the like; Ris cyano, lower alkoxycarbonyl, carboxy or the like, which exhibit potent COMT inhibitory activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.

Catechol derivative, pharmaceutical composition containing the same, use of the catechol derivative, and use of the pharmaceutical composition

The present invention provides compounds represented by general formula (I): or pharmaceutical acceptable salts thereof, wherein Rand Rare each hydrogen, lower acyl, lower alkoxycarbonyl or the like; Ris halo-lower alkyl, lower acyl, halo-lower alkylcarbonyl, cycloalkylcarbonyl, optionally substituted arylcarbonyl, lower alkoxycarbonyl or the like; Ris lower alkyl, halo-lower alkyl, cycloalkyl, lower alkoxy-lower alkyl or the like, which exhibit potent COMT inhibitory activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.

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Azumino, Japan

Yasunori Ueno